Antitumor Activity of Ionic Liquids Based on Ampicillin |
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Authors: | Dr. Ricardo Ferraz Prof. João Costa‐Rodrigues Prof. Maria H. Fernandes Dr. Miguel M. Santos Dr. Isabel M. Marrucho Prof. Luís Paulo N. Rebelo Prof. Cristina Prudêncio Prof. João Paulo Noronha Dr. Željko Petrovski Dr. Luís C. Branco |
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Affiliation: | 1. Departamento de Química, REQUIMTE‐CQFB, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, 2829‐516 Caparica (Portugal);2. Ciências Químicas e das Biomoléculas, Escola Superior de Tecnologia da Saúde do Porto do Instituto Politécnico do Porto, Rua Valente Perfeito?322, 4400‐330 Vila Nova de Gaia (Portugal);3. Laboratório de Farmacologia e Biocompatibilidade Celular, Faculdade de Medicina Dentária, Universidade do Porto, Rua Dr. Manuel Pereira da Silva, 4200‐393 Porto (Portugal);4. Instituto de Tecnologia Química e Biológica, ITQB, Universidade Nova de Lisboa, Av. da República Esta??o Agronómica Nacional, 2780‐157 Oeiras (Portugal);5. Centro de Farmacologia e Biopatologia Química (U38‐FCT), Faculdade de Medicina da Universidade do Porto (FMUP) (Portugal) |
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Abstract: | Significant antiproliferative effects against various tumor cell lines were observed with novel ampicillin salts as ionic liquids. The combination of anionic ampicillin with appropriate ammonium, imidazolium, phosphonium, and pyridinium cations yielded active pharmaceutical ingredient ionic liquids (API‐ILs) that show potent antiproliferative activities against five different human cancer cell lines: T47D (breast), PC3 (prostate), HepG2 (liver), MG63 (osteosarcoma), and RKO (colon). Some API‐ILs showed IC50 values between 5 and 42 nM , activities that stand in dramatic contrast to the negligible cytotoxic activity level shown by the ampicillin sodium salt. Moreover, very low cytotoxicity against two primary cell lines—skin (SF) and gingival fibroblasts (GF)—indicates that the majority of these API‐ILs are nontoxic to normal human cell lines. The most promising combination of antitumor activity and low toxicity toward healthy cells was observed for the 1‐hydroxyethyl‐3‐methylimidazolium–ampicillin pair ([C2OHMIM][Amp]), making this the most suitable lead API‐IL for future studies. |
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Keywords: | active pharmaceutical ingredients ampicillin antitumor agents ionic liquids toxicity |
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